CN115348961B - 杂环pad4抑制剂 - Google Patents
杂环pad4抑制剂 Download PDFInfo
- Publication number
- CN115348961B CN115348961B CN202180025726.9A CN202180025726A CN115348961B CN 115348961 B CN115348961 B CN 115348961B CN 202180025726 A CN202180025726 A CN 202180025726A CN 115348961 B CN115348961 B CN 115348961B
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- CN
- China
- Prior art keywords
- pyridin
- cyclopropylmethyl
- methylpyrazolo
- carbonyl
- amino
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Physical Education & Sports Medicine (AREA)
- Pain & Pain Management (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Luminescent Compositions (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Pyridine Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN202041006146 | 2020-02-12 | ||
| IN202041006146 | 2020-02-12 | ||
| PCT/US2021/017554 WO2021163254A1 (en) | 2020-02-12 | 2021-02-11 | Heterocyclic pad4 inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN115348961A CN115348961A (zh) | 2022-11-15 |
| CN115348961B true CN115348961B (zh) | 2025-03-04 |
Family
ID=74856949
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202180025726.9A Active CN115348961B (zh) | 2020-02-12 | 2021-02-11 | 杂环pad4抑制剂 |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US12473304B2 (https=) |
| EP (1) | EP4103559B1 (https=) |
| JP (1) | JP7711075B2 (https=) |
| KR (1) | KR20220140795A (https=) |
| CN (1) | CN115348961B (https=) |
| AR (1) | AR121299A1 (https=) |
| AU (1) | AU2021219710A1 (https=) |
| BR (1) | BR112022015792A2 (https=) |
| CA (1) | CA3167753A1 (https=) |
| CL (1) | CL2022002148A1 (https=) |
| CO (1) | CO2022011388A2 (https=) |
| IL (1) | IL295506A (https=) |
| MX (1) | MX2022009874A (https=) |
| PE (1) | PE20230679A1 (https=) |
| TW (1) | TW202140477A (https=) |
| WO (1) | WO2021163254A1 (https=) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PH12022551513A1 (en) | 2019-12-20 | 2023-04-24 | Mirati Therapeutics Inc | Sos1 inhibitors |
| WO2021158840A1 (en) | 2020-02-06 | 2021-08-12 | Bristol-Myers Squibb Company | Macrocyclic pad4 inhibitors useful as immunosuppressant |
| TW202140477A (zh) | 2020-02-12 | 2021-11-01 | 美商必治妥美雅史谷比公司 | 雜環ｐａｄ４抑制劑 |
| WO2021222353A1 (en) | 2020-04-30 | 2021-11-04 | Gilead Sciences, Inc. | Macrocyclic inhibitors of peptidylarginine deiminases |
| TW202233174A (zh) | 2020-12-22 | 2022-09-01 | 美商基利科學股份有限公司 | 肽基精胺酸去亞胺酶之抑制劑 |
| WO2022140390A1 (en) | 2020-12-22 | 2022-06-30 | Gilead Sciences, Inc. | Inhibitors of peptidylarginine deiminases |
| KR20260041867A (ko) | 2023-07-21 | 2026-03-27 | 브리스톨-마이어스 스큅 컴퍼니 | Pad4 조정제의 시트룰린화 및 활성을 평가하는 방법 |
| WO2026020127A2 (en) | 2024-07-19 | 2026-01-22 | Bristol-Myers Squibb Company | Methods of assessing citrullination and activity of pad2 modulators |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104470919A (zh) * | 2012-07-26 | 2015-03-25 | 葛兰素集团有限公司 | 作为pad4抑制剂的2-(氮杂吲哚-2-基)苯并咪唑 |
| WO2017100601A1 (en) * | 2015-12-09 | 2017-06-15 | Padlock Therapeutics, Inc. | Aza-benzimidazole inhibitors of pad4 |
| CN107849015A (zh) * | 2015-05-21 | 2018-03-27 | 葛兰素知识产权发展有限公司 | 作为pad4抑制剂的苯并咪唑衍生物 |
| WO2019077631A1 (en) * | 2017-10-18 | 2019-04-25 | Jubilant Biosys Limited | IMIDAZO-PYRIDINE COMPOUNDS FOR USE AS PAD INHIBITORS |
Family Cites Families (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE60007310D1 (de) | 1999-06-04 | 2004-01-29 | Elan Pharma Int Ltd | Zusammensetzungen und methoden zur verhinderung des zelltods |
| MX2007010371A (es) | 2005-02-25 | 2008-01-11 | Tetralogic Pharmaceuticals | Inhibidores dimericos iap. |
| US7825154B2 (en) | 2005-08-12 | 2010-11-02 | The United States Of America As Represented By The Secretary Of The Army | Small molecule inhibitors of botulinum neurotoxins |
| CN101466670B (zh) | 2006-04-07 | 2013-04-17 | 梅特希尔基因公司 | 组蛋白脱乙酰酶抑制剂 |
| US7842713B2 (en) | 2006-04-20 | 2010-11-30 | Pfizer Inc | Fused phenyl amido heterocyclic compounds |
| EP2120952A4 (en) | 2007-01-15 | 2011-09-21 | Us Of America As Represented By The Secretary Of The Army On Behalf Of The U S Army Res Inst Of Infe | ANTIVIRAL COMPOUNDS AND METHODS OF USE |
| US20110052562A1 (en) | 2007-12-19 | 2011-03-03 | The Scripps Research Institute | Benzimidazoles and analogs as rho kinase inhibitors |
| JP2010013386A (ja) | 2008-07-02 | 2010-01-21 | Fujifilm Corp | 染毛剤、染毛方法およびその製造方法 |
| WO2013040528A1 (en) | 2011-09-16 | 2013-03-21 | Microbiotix, Inc. | Antimicrobial compounds |
| WO2013052263A2 (en) | 2011-09-16 | 2013-04-11 | Microbiotix, Inc. | Antifungal compounds |
| CN103030627B (zh) | 2013-01-07 | 2017-11-10 | 中国科学院上海有机化学研究所 | 一种噻吩环/呋喃环‑杂芳环结构的合成方法 |
| WO2014177593A1 (en) | 2013-04-29 | 2014-11-06 | MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. | Amorfrutin analogs as ppargamma-modulators |
| WO2016004513A1 (en) | 2014-07-11 | 2016-01-14 | Simon Fraser University | Anti-bacterial pyruvate kinase modulator compounds, compositions, uses and methods |
| KR101501091B1 (ko) | 2014-09-04 | 2015-03-10 | 주식회사 해치엠엠에이 | 도포용 바닥재의 미끄럼방지 요철형성용 롤러장치 |
| US20180312493A1 (en) | 2015-11-04 | 2018-11-01 | Simon Fraser University | Antibiotic Compounds, Pharmaceutical Formulations Thereof And Methods And Uses Therefor |
| AR107032A1 (es) | 2015-12-09 | 2018-03-14 | Padlock Therapeutics Inc | Inhibidores bicíclicos de pad4 |
| US10654814B2 (en) * | 2015-12-22 | 2020-05-19 | Kancera Ab | Bicyclic hydroxamic acids useful as inhibitors of mammalian histone deacetylase activity |
| CA3015482A1 (en) | 2016-02-23 | 2017-08-31 | Padlock Therapeutics, Inc. | Heteroaryl inhibitors of pad4 |
| WO2018022897A1 (en) | 2016-07-27 | 2018-02-01 | Padlock Therapeutics, Inc. | Covalent inhibitors of pad4 |
| US11026937B2 (en) | 2016-09-12 | 2021-06-08 | Padlock Therapeutics, Inc. | Heteroaryl inhibitors of PAD4 |
| JP2018140974A (ja) | 2017-02-28 | 2018-09-13 | 国立大学法人 奈良先端科学技術大学院大学 | 放射線検出方法及び放射線検出器並びに放射線検出に用いられる新規化合物 |
| CN108689942B (zh) | 2017-04-11 | 2023-06-09 | 广东东阳光药业有限公司 | 含氮双环化合物及其制备方法和用途 |
| JP7311228B2 (ja) * | 2017-06-30 | 2023-07-19 | ベイジン タイド ファーマシューティカル カンパニー リミテッド | Ｒｈｏ－関連プロテインキナーゼ阻害剤、それを含む医薬組成物並びにその調製方法及び使用 |
| ES2932627T3 (es) | 2017-08-22 | 2023-01-23 | Bayer Ag | Derivados heterocíclicos como pesticidas |
| MX2021001565A (es) | 2018-08-08 | 2021-04-19 | Bristol Myers Squibb Co | Inhibidores tipo indol y azaindol de enzimas peptidil arginina deiminasas (pad). |
| MX2021001471A (es) | 2018-08-08 | 2021-04-28 | Bristol Myers Squibb Co | Benzimidazoles sustituidos como inhibidores de peptidil arginina deiminasa 4 (pad4). |
| JP7447080B2 (ja) | 2018-08-08 | 2024-03-11 | ブリストル－マイヤーズ スクイブ カンパニー | Ｐａｄ４阻害剤としての置換チエノピロール |
| US20220348562A1 (en) | 2018-08-08 | 2022-11-03 | Bristol-Myers Squibb Company | Benzimidazole inhibitors of pad enzymes |
| WO2021158840A1 (en) | 2020-02-06 | 2021-08-12 | Bristol-Myers Squibb Company | Macrocyclic pad4 inhibitors useful as immunosuppressant |
| TW202140477A (zh) | 2020-02-12 | 2021-11-01 | 美商必治妥美雅史谷比公司 | 雜環ｐａｄ４抑制劑 |
-
2021
- 2021-02-09 TW TW110105125A patent/TW202140477A/zh unknown
- 2021-02-10 AR ARP210100336A patent/AR121299A1/es not_active Application Discontinuation
- 2021-02-11 US US17/799,028 patent/US12473304B2/en active Active
- 2021-02-11 CN CN202180025726.9A patent/CN115348961B/zh active Active
- 2021-02-11 MX MX2022009874A patent/MX2022009874A/es unknown
- 2021-02-11 CA CA3167753A patent/CA3167753A1/en active Pending
- 2021-02-11 IL IL295506A patent/IL295506A/en unknown
- 2021-02-11 EP EP21709851.6A patent/EP4103559B1/en active Active
- 2021-02-11 PE PE2022001712A patent/PE20230679A1/es unknown
- 2021-02-11 BR BR112022015792A patent/BR112022015792A2/pt not_active Application Discontinuation
- 2021-02-11 KR KR1020227031398A patent/KR20220140795A/ko active Pending
- 2021-02-11 AU AU2021219710A patent/AU2021219710A1/en not_active Abandoned
- 2021-02-11 JP JP2022548707A patent/JP7711075B2/ja active Active
- 2021-02-11 WO PCT/US2021/017554 patent/WO2021163254A1/en not_active Ceased
-
2022
- 2022-08-10 CL CL2022002148A patent/CL2022002148A1/es unknown
- 2022-08-12 CO CONC2022/0011388A patent/CO2022011388A2/es unknown
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104470919A (zh) * | 2012-07-26 | 2015-03-25 | 葛兰素集团有限公司 | 作为pad4抑制剂的2-(氮杂吲哚-2-基)苯并咪唑 |
| CN107849015A (zh) * | 2015-05-21 | 2018-03-27 | 葛兰素知识产权发展有限公司 | 作为pad4抑制剂的苯并咪唑衍生物 |
| WO2017100601A1 (en) * | 2015-12-09 | 2017-06-15 | Padlock Therapeutics, Inc. | Aza-benzimidazole inhibitors of pad4 |
| WO2019077631A1 (en) * | 2017-10-18 | 2019-04-25 | Jubilant Biosys Limited | IMIDAZO-PYRIDINE COMPOUNDS FOR USE AS PAD INHIBITORS |
Non-Patent Citations (1)
| Title |
|---|
| Synthesis of reversible PAD4 inhibitors via copper-catalyzed C−H arylation of benzimidazole;Zhengwei Guo等;《Sci China Chem》;第62卷(第5期);592-596 * |
Also Published As
| Publication number | Publication date |
|---|---|
| AU2021219710A1 (en) | 2022-10-06 |
| US12473304B2 (en) | 2025-11-18 |
| EP4103559B1 (en) | 2026-03-04 |
| JP2023515780A (ja) | 2023-04-14 |
| US20230167131A1 (en) | 2023-06-01 |
| AR121299A1 (es) | 2022-05-04 |
| KR20220140795A (ko) | 2022-10-18 |
| EP4103559A1 (en) | 2022-12-21 |
| PE20230679A1 (es) | 2023-04-21 |
| CA3167753A1 (en) | 2021-08-19 |
| JP7711075B2 (ja) | 2025-07-22 |
| TW202140477A (zh) | 2021-11-01 |
| MX2022009874A (es) | 2022-08-22 |
| BR112022015792A2 (pt) | 2022-10-11 |
| WO2021163254A1 (en) | 2021-08-19 |
| IL295506A (en) | 2022-10-01 |
| CN115348961A (zh) | 2022-11-15 |
| CO2022011388A2 (es) | 2022-08-30 |
| CL2022002148A1 (es) | 2023-02-24 |
| EP4103559C0 (en) | 2026-03-04 |
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